Toremifene

drugbox
IUPAC_name = 2- [4-(4-chloro-1, 2-diphenyl-but-1-enyl)phenoxy] - "N","N"-dimethyl-ethanamine

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CAS_number = 89778-26-7
ATC_prefix = L02
ATC_suffix = BA02
ATC_supplemental =
PubChem = 3005573
DrugBank = APRD00391
C = 26 | H = 28 | Cl = 1 | N = 1 | O = 1
molecular_weight = 405.959 g/mol
bioavailability =
protein_bound = more than 99.5%
metabolism =
elimination_half-life = 5 days
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category =
legal_AU =
legal_UK =
legal_US =
legal_status =
routes_of_administration =

Toremifene citrate is an oral selective estrogen receptor modulator (SERM) which helps oppose the actions of estrogen in the body. Licensed in the United States under the brand name Fareston, toremifene citrate is FDA approved for use in advanced (metastatic) breast cancer. It is also being evaluated for prevention of prostate cancer under the brand name Acapodene. [Price N, Sartor O, Hutson T, Mariani S. Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer. "Clin Prostate Cancer" 2005;3:211-4. PMID 15882476]

[http://www.gtxinc.com GTx Inc.] is currently conducting two different phase 3 clinical trials; First, a pivotal Phase clinical trial for the treatment of serious side effects of androgen deprivation therapy (especially vertebral/spine fractures and hot flashes, lipid profile, and gynecomastia) for advanced prostate cancer, and second, a pivotal Phase III clinical trial for the prevention of prostate cancer in high risk men with high grade prostatic intraepithelial neoplasia, or PIN. Results of these trials are expected by first quarter of 2008 [cite press release
title = GTx's Phase III Clinical Development of ACAPODENE on Course Following Planned Safety Review
publisher = GTx Inc.
date = 2007-07-12
url = http://phx.corporate-ir.net/phoenix.zhtml?c=148196&p=irol-newsArticle&ID=1025420&highlight=
accessdate = 2006-07-14 ]

References